Production of antibiotic micro- and nano-particles by supercritical antisolvent precipitation
Production of antibiotic micro- and nano-particles by supercritical antisolvent precipitation
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DOI：
10.1016/s0032-5910(99)00062-5
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发表时间：
1999-11
影响因子：
5.2
通讯作者：
E. Reverchon;G. Porta
中科院分区：
文献类型：
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作者：
E. Reverchon;G. Porta
超临界抗溶剂沉淀法(SAS)已被用于生产某些抗生素的微粉化颗粒。灰黄霉素、氨苄西林、阿莫西林和四环素已经在N-甲基吡咯烷酮、二甲基亚砜、乙醇和二氯甲烷中进行了测试。已成功地处理了一些抗生素-液体耦合溶剂。在所有成功的SAS条件下都得到了非晶态颗粒，而当微粉化过程失败时，有时会观察到结晶。例如，在N-甲基吡咯烷酮中观察到了四环素的球形纳米颗粒。这些颗粒倾向于聚集成小的聚集体。研究了SAS工艺参数对四环素/N-甲基吡咯烷酮共混体系的形态、粒径和粒径分布的影响。四环素颗粒的聚集度随着操作压力的增加而减小，而聚集体的直径则随着四环素在液体溶剂中的浓度而增大。在180bar、40°C和不同浓度下，观察到平均直径在0.6~0.8μm之间的聚集体。
Supercritical antisolvent precipitation (SAS) has been used to produce micronized particles of some antibiotics. Griseofulvin, ampicillin, amoxicillin, and tetracycline have been tested in N-methylpyrrolidone, dimethylsulfoxide, ethyl alcohol and methylene chloride. Some coupled antibiotic–liquid solvent have been successfully processed. Amorphous particles have been obtained at all successful SAS conditions while crystals have been sometimes observed when the micronization process failed. For example, spherical nanoparticles have been observed for tetracycline in N-methylpyrrolidone. These particles tend to coalesce in small aggregate-forming groups. The effect of the SAS process parameters on morphology, particle size and particle size distribution have been studied for the system tetracycline/N-methylpyrrolidone. The coalescence of tetracycline particles decreases with the increase in operating pressure; whereas the diameter of the aggregates increases with tetracycline concentration in the liquid solvent. Operating at 180 bar, 40°C and at different concentrations, aggregates with mean diameters between 0.6 and 0.8 μm have been observed.